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A kind of nanoparticle loaded with camptothecin drugs of human serum albumin and its preparation method and application

A drug-loaded nanometer and albumin technology, which is applied in the field of anti-tumor drugs, can solve the problems of affecting the curative effect, low conversion yield, and short maintenance time of blood drug concentration.

Inactive Publication Date: 2019-02-26
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, SN38 is insoluble in water and pharmaceutically acceptable solvents (such as Tween or polyoxyethylene castor oil), so it cannot be directly used for clinical injection
After its water-soluble derivative irinotecan (CPT-11) enters the body, it is unstable, eliminated quickly, and has a short blood concentration maintenance time; in addition, the transformation into SN38 with therapeutic effect in vivo depends on the activity of carboxylesterase, and its conversion Productivity is lower than 8%, seriously affects its curative effect
At present, there is no report on the use of albumin as a carrier of camptothecin antineoplastic drugs

Method used

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  • A kind of nanoparticle loaded with camptothecin drugs of human serum albumin and its preparation method and application
  • A kind of nanoparticle loaded with camptothecin drugs of human serum albumin and its preparation method and application
  • A kind of nanoparticle loaded with camptothecin drugs of human serum albumin and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0040] The synthesis method of RA-SN38 refers to the applicant's previous patent "An all-trans retinoic acid-camptothecin anticancer drug conjugate and its preparation method and application", the patent application number or patent number is 201410692682.7.

[0041] Synthetic route such as figure 1 shown.

Embodiment 2

[0043] The synthesis method of linoleic acid-SN38 refers to the applicant's previous patent "7-ethyl-10-hydroxycamptothecin prodrug and its preparation method and application", and the patent application number is 201410295432.X.

[0044] Synthetic route such as figure 2 shown.

Embodiment 3

[0046] The synthesis method of linolenic acid-SN38 refers to the applicant's previous patent "7-ethyl-10-hydroxycamptothecin prodrug and its preparation method and application", and the patent application number is 201410295432.X.

[0047] Synthetic route such as image 3 shown.

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Abstract

The invention discloses nano-particles of human serum albumin loaded camptothecin prodrugs, as well as a preparation method and application thereof. The albumin drug-loaded nano-particles are successfully prepared by adopting a desolvation method, and the method is simple and easy to operate and has good repeatability. The prepared albumin drug-loaded nano-particles have strong capability of inhibiting reproduction of tumor cells, which proves that the albumin drug-loaded nano-particles have a wide anti-tumor application prospect.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, and in particular relates to a preparation method and application of albumin-loaded camptothecin class antitumor drug nanoparticles. Background technique [0002] The use of nanocarriers and related technologies to deliver anticancer drugs is a hot research issue in the field of tumor therapy. The main advantages of nanomedicine are as follows: 1) The endothelial cell gap of tumor blood vessels is relatively loose, and nanoparticles below 200nm can passively enter tumor tissue through the high permeability and retention effect (EPR) of solid tumors. In addition, nanoparticles themselves can be modified by ligand molecules for active targeting. Whether it is active or passive targeting of nanoparticles, the drug can be enriched in tumor tissue, and while increasing the efficacy of the drug, it relatively reduces The dosage of the drug greatly reduces the toxic and side effects of anticancer drugs. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/4745A61K47/42A61P35/00
CPCA61K9/5169A61K31/4745
Inventor 王杭祥陈建美
Owner ZHEJIANG UNIV